LGD-6972 ( LGD6972 | RVT 1502 )

产品货号. M10771 CAS No. 1207989-09-0

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

产品询价大包装询价加入购物车

产品名称

LGD-6972
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

LGD-6972 (RVT 1502) 是一种新型强效、选择性、口服生物可利用的胰高血糖素受体 (GCGR) 拮抗剂。
产品描述

LGD-6972 (RVT 1502) is a novel potent, selective, orally bioavailable glucagon receptor (GCGR) antagonist; binds competitively to GCGR with high affinity and selectivity, suppressing both cAMP and glucose production in vitro; reduces acute glucagon-stimulated hyperglycaemia as well as the hyperglycaemia observed in diabetic mouse models in vivo.Diabetes Phase 2 Clinical.
体外实验

In vitro, LGD-6972 binds competitively to glucagon receptor (GCGR) with high affinity and selectivity, suppressing both cAMP and glucose production.
体内实验

In vivo, LGD-6972 reduces acute glucagon-stimulated hyperglycaemia as well as the hyperglycaemia observed in diabetic mouse models. The pharmacological activity of LGD-6972 appears to be mediated primarily by inhibiting glucagon receptor signaling.
同义词

LGD6972 | RVT 1502
通路

GPCR/G Protein
靶点

Glucagon Receptor
受体

Glucagon Receptor
研究领域

Metabolic Disease
适应症

Diabetes

CAS Number

1207989-09-0
分子量

702.9008
分子式

C43H46N2O5S
纯度

>98% (HPLC)
溶解度

DMSO: ≥ 31 mg/mL
SMILES

CC1=CC(=C(C(=C1)C)C2=CC=C(C=C2)NC(=O)C(CC3=CC=C(C=C3)C(=O)NCCS(=O)(=O)O)C4=CC=C(C=C4)C5=CC=C(C=C5)C(C)(C)C)C
化学全称

Ethanesulfonic acid, 2-[[4-[(2R)-2-[4'-(1,1-dimethylethyl)[1,1'-biphenyl]-4-yl]-3-oxo-3-[(2',4',6'-trimethyl[1,1'-biphenyl]-4-yl)amino]propyl]benzoyl]amino]-

1. Vajda EG, et al. Diabetes Obes Metab. 2017 Jan;19(1):24-32. 2. Vajda EG, et al. Diabetes. 2012;61(suppl 1):A252. Abstract.

计算器

产品手册

关联产品

Bay 55-9837

Selective VPAC2 receptor agonist (EC50 values are 0.4, 100 and >1000 nM for VPAC2, VPAC1 and PAC1, respectively in a cAMP accumulation assay; IC50 values are 60, 8700 and >10000 nM for VPAC2, VPAC1 and PAC1, respectively in a competition binding assay). Stimulates glucose-dependent insulin secretion in isolated human pancreatic islets. Reduces HIV-1 viral replication and shows cooperative effects when given in conjunction with VPAC1 agonists.
NNC 92-1687

NNC 92-1687 is a selective glucagon receptor antagonist that can be used to study type 2 diabetes.
CCG-143140

CCG-143140 是一种 GLP-1 受体反向激动剂。